US10421758B2 - Selective Grp94 inhibitors and uses thereof - Google Patents

Selective Grp94 inhibitors and uses thereof Download PDF

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Publication number
US10421758B2
US10421758B2 US14/912,082 US201414912082A US10421758B2 US 10421758 B2 US10421758 B2 US 10421758B2 US 201414912082 A US201414912082 A US 201414912082A US 10421758 B2 US10421758 B2 US 10421758B2
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US20160194328A1 (en
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Gabriela Chiosis
Pengrong Yan
Pallav Patel
Hardik J. Patel
Tony Taldone
Chenghua Yang
Weilin Sun
Stefan O. Ochiana
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Memorial Sloan Kettering Cancer Center
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/5005—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
    • G01N33/5008—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics
    • G01N33/5011—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics for testing antineoplastic activity
    • G—PHYSICS
    • G16—INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR SPECIFIC APPLICATION FIELDS
    • G16B—BIOINFORMATICS, i.e. INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR GENETIC OR PROTEIN-RELATED DATA PROCESSING IN COMPUTATIONAL MOLECULAR BIOLOGY
    • G16B35/00—ICT specially adapted for in silico combinatorial libraries of nucleic acids, proteins or peptides
    • G—PHYSICS
    • G16—INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR SPECIFIC APPLICATION FIELDS
    • G16C—COMPUTATIONAL CHEMISTRY; CHEMOINFORMATICS; COMPUTATIONAL MATERIALS SCIENCE
    • G16C20/00—Chemoinformatics, i.e. ICT specially adapted for the handling of physicochemical or structural data of chemical particles, elements, compounds or mixtures
    • G16C20/60—In silico combinatorial chemistry
    • G—PHYSICS
    • G16—INFORMATION AND COMMUNICATION TECHNOLOGY [ICT] SPECIALLY ADAPTED FOR SPECIFIC APPLICATION FIELDS
    • G16C—COMPUTATIONAL CHEMISTRY; CHEMOINFORMATICS; COMPUTATIONAL MATERIALS SCIENCE
    • G16C20/00—Chemoinformatics, i.e. ICT specially adapted for the handling of physicochemical or structural data of chemical particles, elements, compounds or mixtures
    • G16C20/60—In silico combinatorial chemistry
    • G16C20/64—Screening of libraries
US14/912,082 2013-08-16 2014-08-15 Selective Grp94 inhibitors and uses thereof Active US10421758B2 (en)

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US201361866932P 2013-08-16 2013-08-16
PCT/US2014/051332 WO2015023976A2 (en) 2013-08-16 2014-08-15 Selective grp94 inhibitors and uses thereof
US14/912,082 US10421758B2 (en) 2013-08-16 2014-08-15 Selective Grp94 inhibitors and uses thereof

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US10421758B2 true US10421758B2 (en) 2019-09-24

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US16/376,614 Active US11267816B2 (en) 2013-08-16 2019-04-05 Selective Grp94 inhibitors and uses thereof
US17/581,010 Pending US20230123747A1 (en) 2013-08-16 2022-01-21 Selective grp94 inhibitors and uses thereof

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US (3) US10421758B2 (pt)
EP (1) EP3033338A4 (pt)
JP (2) JP6539275B2 (pt)
KR (1) KR102319582B1 (pt)
CN (1) CN105899503B (pt)
AU (2) AU2014306417C1 (pt)
BR (1) BR112016003201A2 (pt)
CA (1) CA2921571C (pt)
EA (1) EA201690406A1 (pt)
HK (1) HK1226063A1 (pt)
IL (2) IL244251B (pt)
MX (1) MX370664B (pt)
PH (1) PH12016500511A1 (pt)
SG (2) SG10201801281QA (pt)
TW (1) TWI711618B (pt)
WO (1) WO2015023976A2 (pt)
ZA (1) ZA201601794B (pt)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20200102312A1 (en) * 2013-08-16 2020-04-02 Memorial Sloan-Kettering Cancer Center Selective grp94 inhibitors and uses thereof
US10793570B2 (en) 2013-12-23 2020-10-06 Memorial Sloan-Kettering Cancer Center Methods and reagents for radiolabeling
US11260132B2 (en) * 2017-03-16 2022-03-01 Children's Medical Center Corporation Engineered liposomes as cancer-targeted therapeutics

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9403828B2 (en) 2005-02-01 2016-08-02 Sloan-Kettering Institute For Cancer Research Small-molecule Hsp90 inhibitors
US7834181B2 (en) 2005-02-01 2010-11-16 Slaon-Kettering Institute For Cancer Research Small-molecule Hsp90 inhibitors
US10336757B2 (en) 2006-06-30 2019-07-02 Sloan-Kettering Institute For Cancer Research Treatment of neurodegenerative diseases through inhibition of HSP90
NZ599138A (en) 2009-10-07 2014-06-27 Sloan Kettering Inst Cancer Purine derivatives useful as hsp90 inhibitors
CN103582642B (zh) 2011-04-05 2021-05-11 索隆-基特林癌症研究协会 Hsp90抑制剂
AU2012240079B2 (en) 2011-04-05 2017-05-18 Sloan-Kettering Institute For Cancer Research Hsp90 inhibitors
TWI721929B (zh) * 2013-08-05 2021-03-11 美商扭轉生物科技有限公司 重新合成之基因庫
CA2961499A1 (en) 2014-09-17 2016-03-24 Memorial Sloan Kettering Cancer Center Hsp90-targeted inflammation and infection imaging and therapy
WO2017062520A1 (en) 2015-10-05 2017-04-13 Memorial Sloan Kettering Cancer Center Rational combination therapy for the treatment of cancer
CN108503643B (zh) * 2017-02-28 2020-09-15 泉州易初生物医药科技有限公司 蛋白酶抑制剂的制备方法
WO2019136093A1 (en) * 2018-01-02 2019-07-11 Sanford Burnham Prebys Medical Discovery Institute Inhibitors of low molecular weight protein tyrosine phosphatase (lmptp) and uses thereof
US11774451B2 (en) * 2019-11-21 2023-10-03 The Board Of Trustees Of The Leland Stanford Junior University Molecular vibrational spectroscopic markers for detection of cancer
WO2021251564A1 (ko) * 2020-06-09 2021-12-16 국민대학교산학협력단 Grp94에 특이적으로 결합하는 항체 또는 그의 항원 결합 단편 및 이들의 용도
KR20230000050A (ko) 2021-06-24 2023-01-02 최현지 페이크 마스크
CN113663078B (zh) * 2021-06-28 2023-05-16 四川大学 Grp94抑制剂在制备治疗EGFR驱动的癌症的药物中的用途
KR20240012846A (ko) 2022-07-21 2024-01-30 성균관대학교산학협력단 신규한 hdac6 선택적 억제제 및 이의 용도
CN115717144A (zh) * 2022-08-25 2023-02-28 南通市肿瘤医院 抑制hsp90b1表达的小干扰rna及其在膀胱癌衰老中的应用

Citations (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995002597A1 (en) 1993-07-15 1995-01-26 Minnesota Mining And Manufacturing Company IMIDAZO[4,5-c]PYRIDIN-4-AMINES
WO2003037860A2 (en) 2001-10-30 2003-05-08 Conforma Therapeutics Corporation Purine analogs having hsp90-inhibiting activity
US20040102458A1 (en) 2000-11-02 2004-05-27 Gabriela Chiosis Small molecule compositions for binding to hsp90
US20050107343A1 (en) 2003-09-18 2005-05-19 Conforma Therapeutics Corporation Pyrrolopyrimidines and related analogs as HSP90-inhibitors
US20050256183A1 (en) 2001-11-09 2005-11-17 Kasibhatla Srinivas R Hsp90-inhibiting zearalanol compounds and methods of producing and using same
WO2006084030A2 (en) 2005-02-01 2006-08-10 Sloan-Kettering Institute For Cancer Research Small-molecule hsp90 inhibitors
WO2007075572A2 (en) 2005-12-22 2007-07-05 Conforma Therapeutics Corporation Orally active purine-based inhibitors of heat shock protein 90
WO2007134298A2 (en) 2006-05-12 2007-11-22 Myriad Genetics, Inc. Therapeutic compounds and their use in cancer
WO2008005937A2 (en) 2006-06-30 2008-01-10 Sloan-Kettering Institute For Cancer Research Treatment of neurodegenerative diseases through inhibiton of hsp90
WO2008115719A1 (en) 2007-03-20 2008-09-25 Curis, Inc. Fused amino pyridine as hsp90 inhibitors
US20100015128A1 (en) 2006-10-03 2010-01-21 University Of Southern California GRP78 as a Predictor of Responsiveness to Therapeutic Agents
WO2011044394A1 (en) 2009-10-07 2011-04-14 Sloan-Kettering Institute For Cancer Research Purine derivatives useful as hsp90 inhibitors
US20110312980A1 (en) 2005-02-01 2011-12-22 Sloan-Kettering Institute For Cancer Research Small-molecule Hsp90 Inhibitors
US20120022070A1 (en) 2008-10-06 2012-01-26 Emory University Heat Shock Protein 90 Inhibitors, Methods Of Preparing Same, And Methods For Their Use
WO2012138896A1 (en) 2011-04-05 2012-10-11 Sloan-Kettering Institute For Cancer Research Hsp90 inhibitors
WO2012138894A1 (en) 2011-04-05 2012-10-11 Sloan-Kettering Institute For Cancer Research Hsp90 inhibitors
WO2013009657A1 (en) 2011-07-08 2013-01-17 Sloan-Kettering Institute For Cancer Research Uses of labeled hsp90 inhibitors
US20130109684A1 (en) 2011-04-08 2013-05-02 University Of Kansas Grp94 inhibitors

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070129334A1 (en) * 2001-10-30 2007-06-07 Conforma Therapeutics Corporation Orally Active Purine-Based Inhibitors of Heat Shock Protein 90
CA2705579A1 (en) 2007-11-14 2009-05-22 Myriad Pharmaceuticals, Inc. Therapeutic compounds and their use in treating diseases and disorders
US20140335050A1 (en) 2011-05-27 2014-11-13 The General Hospital Corporation Methods, compositions, and kits for the treatment of cancer
AU2014306417C1 (en) 2013-08-16 2019-07-25 Memorial Sloan-Kettering Cancer Center Selective Grp94 inhibitors and uses thereof

Patent Citations (51)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995002597A1 (en) 1993-07-15 1995-01-26 Minnesota Mining And Manufacturing Company IMIDAZO[4,5-c]PYRIDIN-4-AMINES
US20040102458A1 (en) 2000-11-02 2004-05-27 Gabriela Chiosis Small molecule compositions for binding to hsp90
CN1501928A (zh) 2000-11-02 2004-06-02 斯隆-凯特林癌症研究所 结合hsp90的小分子组合物
US7439359B2 (en) 2000-11-02 2008-10-21 Sloan-Kettering Institute For Cancer Research Small molecule compositions for binding to hsp90
WO2003037860A2 (en) 2001-10-30 2003-05-08 Conforma Therapeutics Corporation Purine analogs having hsp90-inhibiting activity
US20050049263A1 (en) 2001-10-30 2005-03-03 Kasibhatla Srinivas Rao Purine analogs having hsp90-inhibiting activity
US7241890B2 (en) 2001-10-30 2007-07-10 Conforma Therapeutics Corporation Purine analogs having HSP90-inhibiting activity
US20050256183A1 (en) 2001-11-09 2005-11-17 Kasibhatla Srinivas R Hsp90-inhibiting zearalanol compounds and methods of producing and using same
US20050113340A1 (en) 2003-09-18 2005-05-26 Conforma Therapeutics Corporation 2-Aminopurine analogs having HSP90-inhibiting activity
US20050113339A1 (en) 2003-09-18 2005-05-26 Kasibhatla Srinivas R. Triazolopyrimidines and related analogs as HSP90-inhibitors
US20050107343A1 (en) 2003-09-18 2005-05-19 Conforma Therapeutics Corporation Pyrrolopyrimidines and related analogs as HSP90-inhibitors
US20160333014A1 (en) 2005-02-01 2016-11-17 Sloan-Kettering Institute For Cancer Research Small-molecule hsp90 inhibitors
US10000494B2 (en) 2005-02-01 2018-06-19 Sloan-Kettering Institute For Cancer Research Small-molecule Hsp90 inhibitors
US20190023708A1 (en) 2005-02-01 2019-01-24 Sloan-Kettering Institute For Cancer Research Small-molecule hsp90 inhibitors
US10167285B2 (en) 2005-02-01 2019-01-01 Memorial Sloan Kettering Cancer Center Small-molecule HSP90 inhibitors
US20080253965A1 (en) 2005-02-01 2008-10-16 Sloan-Kettering Institute For Cancer Research Small-Molecule Hsp90 Inhibitors
US20140227183A1 (en) 2005-02-01 2014-08-14 Memorial Sloan Kettering Cancer Center Small-molecule hsp90 inhibitors
US20110312980A1 (en) 2005-02-01 2011-12-22 Sloan-Kettering Institute For Cancer Research Small-molecule Hsp90 Inhibitors
US8703942B2 (en) * 2005-02-01 2014-04-22 Sloan-Kettering Institute For Cancer Research Small-molecule Hsp90 inhibitors
US20170342073A1 (en) 2005-02-01 2017-11-30 Memorial Sloan Kettering Cancer Center Small-molecule hsp90 inhibitors
US9701678B2 (en) 2005-02-01 2017-07-11 Memorial Sloan Kettering Cancer Center Small-molecule HSP90 inhibitors
WO2006084030A2 (en) 2005-02-01 2006-08-10 Sloan-Kettering Institute For Cancer Research Small-molecule hsp90 inhibitors
US7834181B2 (en) * 2005-02-01 2010-11-16 Slaon-Kettering Institute For Cancer Research Small-molecule Hsp90 inhibitors
US9403828B2 (en) * 2005-02-01 2016-08-02 Sloan-Kettering Institute For Cancer Research Small-molecule Hsp90 inhibitors
US20110104054A1 (en) 2005-02-01 2011-05-05 Sloan-Kettering Institute For Cancer Research Small-Molecule HSP90 Inhibitors
JP2009521446A (ja) 2005-12-22 2009-06-04 コンフォーマ・セラピューティクス・コーポレイション 熱ショックタンパク質９０の経口活性なプリンベースの阻害剤
WO2007075572A2 (en) 2005-12-22 2007-07-05 Conforma Therapeutics Corporation Orally active purine-based inhibitors of heat shock protein 90
WO2007134298A2 (en) 2006-05-12 2007-11-22 Myriad Genetics, Inc. Therapeutic compounds and their use in cancer
CN101490052A (zh) 2006-05-12 2009-07-22 美瑞德生物工程公司 治疗性化合物及其在癌症中的用途
US20100016586A1 (en) 2006-05-12 2010-01-21 Myriad Genetics, Incorporated Therapeutic compounds and their use in cancer
WO2008005937A2 (en) 2006-06-30 2008-01-10 Sloan-Kettering Institute For Cancer Research Treatment of neurodegenerative diseases through inhibiton of hsp90
US20090298857A1 (en) 2006-06-30 2009-12-03 Sloan-Kettering Institute For Cancer Research Treatment of Neurodegenerative Diseases Through Inhibition of HSP90
US20140378452A1 (en) 2006-06-30 2014-12-25 Sloan-Kettering Institute For Cancer Research Treatment of Neurodegenerative Diseases Through Inhibition of HSP90
US20100015128A1 (en) 2006-10-03 2010-01-21 University Of Southern California GRP78 as a Predictor of Responsiveness to Therapeutic Agents
WO2008115719A1 (en) 2007-03-20 2008-09-25 Curis, Inc. Fused amino pyridine as hsp90 inhibitors
US20120022070A1 (en) 2008-10-06 2012-01-26 Emory University Heat Shock Protein 90 Inhibitors, Methods Of Preparing Same, And Methods For Their Use
US20160310497A1 (en) 2009-10-07 2016-10-27 Sloan-Kettering Institute For Cancer Research Purine derivatives useful as hsp90 inhibitors
US10172863B2 (en) 2009-10-07 2019-01-08 Sloan-Kettering Institute For Cancer Research Purine derivatives useful as HSP90 inhibitors
US9328114B2 (en) 2009-10-07 2016-05-03 Sloan-Kettering Institute For Cancer Research Hsp90 inhibitors
WO2011044394A1 (en) 2009-10-07 2011-04-14 Sloan-Kettering Institute For Cancer Research Purine derivatives useful as hsp90 inhibitors
WO2012138896A1 (en) 2011-04-05 2012-10-11 Sloan-Kettering Institute For Cancer Research Hsp90 inhibitors
US20160264577A1 (en) 2011-04-05 2016-09-15 Sloan-Kettering Institute For Cancer Research Hsp90 inhibitors
US9546170B2 (en) 2011-04-05 2017-01-17 Sloan-Kettering Institute For Cancer Research Hsp90 inhibitors
US20170151247A1 (en) 2011-04-05 2017-06-01 Sloan-Kettering Institute For Cancer Research Hsp90 inhibitors
US9346808B2 (en) 2011-04-05 2016-05-24 Sloan-Kettering Institute For Cancer Research Hsp90 inhibitors
WO2012138894A1 (en) 2011-04-05 2012-10-11 Sloan-Kettering Institute For Cancer Research Hsp90 inhibitors
US9926321B2 (en) 2011-04-05 2018-03-27 Sloan-Kettering Institute For Cancer Research Hsp90 inhibitors
US20140088121A1 (en) 2011-04-05 2014-03-27 Sloan-Kettering Institute For Cancer Research HSP90 Inhibitors
US20130109684A1 (en) 2011-04-08 2013-05-02 University Of Kansas Grp94 inhibitors
WO2013009655A2 (en) 2011-07-08 2013-01-17 Sloan-Kettering Institute For Cancer Research Uses of labeled hsp90 inhibitors
WO2013009657A1 (en) 2011-07-08 2013-01-17 Sloan-Kettering Institute For Cancer Research Uses of labeled hsp90 inhibitors

Non-Patent Citations (74)

* Cited by examiner, † Cited by third party
Title
Ali, M. M. et al. Crystal structure of an Hsp90-nucleotide-p23/Sbal closed chaperone complex, Nature 440, 1013-1017 (2006).
Andrews, D. et al., Results of a pilot study involving the use of an antisense oligodeoxynucleotide directed against the insulin-like growth factor type I receptor in malignant astrocytomas, J. Clin. Oncol., 19(8):2189-200 (2001).
Arteaga, C. et al., Growth inhibition of human breast cancer cells in vitro with an antibody against the type I somatomedin receptor, Cancer Res., 49(22):6237-41 (1989).
Author Unknown, 1H-benzimidazole-1-acetamide, 4-amino-2-(phenylmethyl)-, CAS RN 1216054-06-6, STN Entry Date Apr. 4, 2010.
Author Unknown, 1H-benzimidazole-1-acetamide, 4-amino-2-[(4-fluorophenyl)methyl]-, CAS RN 1216006-29-9, STN Entry Date Apr. 4, 2010.
Author Unknown, 1H-benzimidazole-1-acetic acid hydrazide, 4-amino-2-(phenylmethyl)-, CAS RN 1216116-95-8, STN Entry Date Apr. 4, 2010.
Author Unknown, 1H-benzimidazole-1-propanamine, 4-amino-N,N-dimethyl-2-(phenylmethyl)-, CAS RN 1216041-15-4, STN Entry Date Apr. 4, 2010.
Author Unknown,1H-benzimidazole-1-acetamide, 4-amino-N-methyl-2-(phenylmethyl)-, CAS RN 1216259-68-5, STN Entry Date Apr. 4, 2010.
Author Unknown,1H-benzimidazole-1-ethanamine, 4-amino-N,N-dimethyl-2-(phenylmethyl)-, CAS RN 1216217-64-9, STN Entry Date Apr. 4, 2010.
Bartlett et al, Transforming growth factor-beta mRNA expression and growth control of human ovarian carcinoma cells, Brit. J. Cancer, 65(5):655-60 (1992).
Baserga, R., et al., The IGF-1 receptor in cancer biology, Int. J. Cancer; 107:873-7 (2003).
Biamonte, M.A. et al., Preparation of 8-(Arylsulfanyl) adenines with Diazonium Salts under Mild, Aerobic Conditions, Journal of Organic Chemistry, 70(2):717-720 (2005).
Buck, E. et al, Inactivation of Akt by the epidermal growth factor receptor inhibitor erlotinib is mediated by HER-3 in pancreatic and colorectal tumor cell lines and contributes to erlotinib sensitivity, Mol Cancer Ther, 5:2051-2059 (2006).
Caldas-Lopes, E. et al., Hsp90 inhibitor PU-H71, a multimodal inhibitor of malignancy, induces complete responses in triple-negative breast cancer models, Proc. Natl. Acad. Sci. USA, 106: 8368-73 (2009).
Chavany, C. et al., pI85erbB2 binds to GRP94 in vivo Dissociation of the pI85erbB2/GRP94 heterocomplex by benzoquinone ansamycins precedes depletion of pI85erbB2, J. Biol. Chem, 271: 4974-4977 (1996).
Chen, B. et al., The HSP90 family of genes in the human genome: Insights into their divergence and evolution, Genomics, 86: 627-637 (2005).
Chene, P. et al, ATPases as drug targets: learning from their structure, Nat. Rev. Drug Discov., 1: 665-673 (2002).
Cheng, J-C, et al, TGF-Beta Induces Serous Borderline Ovarian Tumor Cell Invasion by Activating EMT butTriggers Apoptosis in Low-Grade Serous Ovarian Carcinoma Cells, PLoS ONE, 7(8): e42436. doi: 10.1371 (2012).
Chiosis et al. (AN 2011:1656071, DN 156:92369, ZCAPLUS, abstract of U.S. Pat. No. 9,403,828). *
D'Ambrosio, C. et al., A soluble insulin-like growth factor I receptor that induces apoptosis of tumor cells in vivo and inhibits tumorigenesis, Cancer Res, 56(17): 4013-20 (1996).
Dickey, C.A. et al., Development of a high throughput drug screening assay for the detection of changes in tau levels-proof of concept with HSP90 inhibitors, Curr. Alzheimer Res., 2(2):231-8 (2005).
Dickey, C.A. et al., Development of a high throughput drug screening assay for the detection of changes in tau levels—proof of concept with HSP90 inhibitors, Curr. Alzheimer Res., 2(2):231-8 (2005).
Dollins, D. E., et al, Structure of unliganded GRP94, the endoplasmic reticulum Hsp90. Basis for nucleotide-induced conformational change, J. Biol. Chem., 280:30438-30447 (2005).
Dollins, D.E., et al, Structures of GRP94-nucleotide complexes reveal mechanistic differences between the hsp90 chaperones, Mol. Cell, 28:41-56 (2007).
Duerfeldt, A.S., et al, Development of a Grp94 inhibitor, J.Am. Chem. Soc., 134:9796-9804 (2012).
Dymock, B. W., et al., Inhibitors of HSP90 and other chaperones for the treatment of cancer, Expert Opinion, Ther. Patents, 14(6): 837-0847 (2004).
Ferraro, D. et al., Inhibition of triple-negative breast cancer models by combinations of antibodies to EGFR, Proc. Natl. Acad. Sci. USA., 110(5): 1815-20 (2013).
Frey, S. et al, The ATPase cycle of the endoplasmic chaperone Grp94, J. Biol. Chem, 282:35612-35620 (2007).
Friesner, R.A. et al, Extra precision glide: Docking and scoring incorporating a model of hydrophobic enclosure for protein-ligand complexes, J. Med. Chem, 49:6177-6196 (2006).
Friesner, R.A. et al., Glide: a new approach for rapid, accurate docking and scoring. 1. Method and assessment of docking accuracy, J. Med. Chem, 47:1739-49 (2004).
Garcia-Echeverria, C. et al., In vivo antitumor activity of NVP-AEW541-A novel, potent, and selective inhibitor of the IGF-IR kinase, Cancer Cell, 5(3):231-9 (2004).
Garcia-Echeverria, C. et al., In vivo antitumor activity of NVP-AEW541—A novel, potent, and selective inhibitor of the IGF-IR kinase, Cancer Cell, 5(3):231-9 (2004).
Halgren, T. et al, New method for fast and accurate binding-site identification and analysis, Chemical Biology & Drug Design, 69:146-148 (2007).
Halgren, T.A. et al, Glide: a new approach for rapid, accurate docking and scoring. 2. Enrichment factors in database screening, J. Med. Chem., 47:1750-1759 (2004).
Halgren, T.A. et al,. Identifying and Characterizing Binding Sites and Assessing Druggability, J. Chem. Information and Modeling, 49:377-389 (2009).
He, H. et al. Identification of potent water soluble purine-scaffold inhibitors of the heat shock protein 90, J. Med.Chem, 49:381-90 (2006).
Immormino, R. M. et al, Different poses for ligand and chaperone in inhibitor-bound Hsp90 and GRP94: implications for paralog-specific drug design, J. Mal. Biol., 388:1033-1042 (2009).
Immormino, R. M. et al, Structural and quantum chemical studies of 8-aryl-sulfanyl adenine class Hsp90 inhibitors, J. Med. Chem, 49:4953-4960 (2006).
Immormino, R.M. et al., Ligand-induced conformational shift in the N-terminal domain of GRP94, an Hsp90 chaperone, J. Biol. Chem., 279(44):46162-71 (2004).
International Search Report for PCT/US2014/051332, 7 pages (dated Feb. 18, 2015).
Jhaveri, K., et al, Advances in the clinical development of heat shock protein 90(Hsp90) inhibitors in cancers, Biochim. Biophys. Acta., 1823:742-755 (2012).
Johnson, J. L. et al, Evolution and function of diverse Hsp90 homologs and cochaperone proteins, Biochim. Biophys. Acta., 1823:607-613 (2012).
Kang, J. et al., Inhibition of neuroblastoma xenograft growth by HSP90 inhibitors, Anticancer Res., 26(3A):1903-8 (2006).
Kim, T.E. & Murren, J.R., Lapatinib Ditosylate GlaxoSmithKline, IDrugs 6, 886-893 (2003).
Leroith, D. et al., The insulin-like growth factor system and cancer, Cancer Lett., 195(2): 127-37 (2003).
Leskovar, A., et al, The ATPase cycle of the mitochondrial Hsp90 analog Trapl, J. Biol. Chem, 283: 11677-11688 (2008).
Llaugher, L. et al., Evaluation of 8-Arylsulfanyl, 8-Arylsulfonyl Adenine Derivatives as Inhibitors of the Heat Shock Protein 90, J. Med. Chem., 48: 2892-2905 (2005).
Long, L., et al., Loss of the metastatic phenotype in murine carcinoma cells expressing an antisense RNA to the insulin-like growth factor receptor, Cancer Res, 55(5): 1006-9 (1995).
Lucas, B. et al., Facile Synthesis of a Library of 9-Alkyl-8-benzyl-9H-purin-6-ylamine Derivatives, J. Comb. Chem., 3: 518-520 (2001).
Marzec, M. et al, GRP94: An HSP90-like protein specialized for protein folding and quality control in the endoplasmic reticulum, Biochim. Biophys. Acta., 1823:774-787 (2012).
McLaughlin, S. H.et al, Independent ATPase activity of Hsp90 subunits creates a flexible assembly platform, J. Mal. Biol, 344:813-826 (2004).
Moulick, K. et al. Affinity-based proteomics reveal cancer-specific networks coordinated by Hsp90, Nat. Chem. Biol., 7:818-26 (2011).
Mueller et al., Fibroblast-secreted hepatocyte growth factor mediates epidermal growth factor receptor tyrosine kinase inhibitor resistance in triple-negative breast cancers through paracrine activation of Met, Breast Cancer Res., 14( 4):R104 (2012).
Ostrovsky, O. et al, The chaperone activity of GRP94 toward insulinlike growth factor II is necessary for the stress response to serum deprivation, Mal. Biol. Cell, 20:1855-1864 (2009).
Patel, P. D. et al, Paralog-selective Hsp90 inhibitors define tumor-specific regulation of HER2, Nature Chemical Biology, 9: 677-684 (2013).
Pearl, L. H.et al, The Hsp90 molecular chaperone: an open and shut case for treatment, Biochem. J., 410:439-453 (2008).
Pietrzkowski, Z. et al., Inhibition of growth of prostatic cancer cell lines by peptide analogues of insulin-like growth factor 1, Cancer Res., 53(5):1102-6 (1993).
Richter, K. et al, Conserved conformational changes in the ATPase cycle of human hsp90, J. Biol. Chem., 283:17757-17765 (2008).
Rodina, A. et al., Selective compounds define Hsp90 as a major inhibitor of apoptosis in small-cell lung cancer, Nat. Chem. Biol., 3:498-507 (2007).
Schulte, T.W. et al., Interaction of radicicol with members of the heat shock protein 90 family of molecular chaperones, Mol. Endo., 13:1435-1448 (1999).
Siwak, D. et al, Targeting the Epidermal Growth Factor Receptor in Epithelial Ovarian Cancer: Current Knowledge and Future Challenges, Journal of Oncology, 2010; doi:l0.1155/2010/568938).
Sokolowska, I. et al. Proteomic analysis of plasma membranes isolated from undifferentiated and differentiated HepaRG cells, Proteome Sci., 10, 4 7 (2012).
Soldano, K. L. et al, Structure of the N-terminal domain of GRP94: Basis for ligand specificity and regulation, J. Biol. Chem, 279:48330-48338 (2003).
Sreedhar, A. S. et al, Hsp90 isoforms: functions, expression and clinical importance, FEBS letters, 562:11-15 (2004).
Wanderling, S. et al., GRP94 is essential for mesoderm induction and muscle development because it regulates insulin-like growth factor secretion, Mol. Biol. Cell, 18:3764-75 (2007).
Wittman, M., et al., Discovery of a 1H-Benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) Inhibitor of Insulin-like Growth Factor I Receptor Kinase with in Vivo Antitumor Activity, J. Med. Chem., 48(18):5639-43 (2005).
Workman, P.et al, Drugging the cancer chaperone Hsp90: combinatorial therapeutic exploitation of oncogene addiction and tumor stress, Ann. NY. Acad. Sci., 1113: 202-216 (2007).
Written Opinion for PCT/US2014/051332, 8 pages (dated Feb. 18, 2015).
Xu, W. et al, Hsp90, not Grp94, regulates the intracellular trafficking and stability of nascent ErbB2, Cell Stress Chaperones, 7:91-96 (2002).
Yang, Y. et al. Heat shock protein gp96 is a master chaperone for toll-like receptors and is important in the innate function of macrophages, Immunity 26, 215-26 (2007).
Yarden, Y. & Sliwkowski, M. X., Untangling the ErbB signaling network, Nat. Rev. Mal. Cell Biol., 2:127-137 (2001).
Yun, T. J et al, EC144, a Synthetic Inhibitor of Heat Shock Protein 90, Blocks Innate and Adaptive Immune Responses in Models of Inflammation and Autoimmunity, The Journal of Immunology, 186: 563-575 (2011).
Zhang, H. et al, Identification of new biomarkers for clinical trials of HSP90 inhibitors, Molecular Cancer Therapeutics, 5(5): 1256-1264 (2006).
Zhang, L.et al, EGFR and ErbB2 differentially regulate Raf-1 translocation and activation, Lab. Invest., 82:71-78 (2002).

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